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Compound Detail

CHEMBL1078411

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N#C[C@@]1(NC(=O)[C@@H](N)Cc2cccs2)C[C@@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL1078411
Phase Preclinical
Structure Type MOL
InChI Key FUYOZZGSCQXNCB-VYDXJSESSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
14
Publications
0
Known Names

Molecular Properties

311.4
MW (Da)
2.18
ALogP
4
HBA
2
HBD
78.9
PSA (Ų)
0.89
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17N3OS
MW 311.41
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.62

Activity Summary

IC50 3 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 1
CHEMBL2252
IC50 7.85 7.85 14.0 1
Procathepsin L
CHEMBL3837
IC50 5.27 5.27 5400.0 1
Cathepsin S
CHEMBL2954
IC50 5.23 5.23 5900.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 1.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 1 IC50 = 14.0 nM 7.85 Inhibition of human recombinant cathepsin C 19665376
Procathepsin L IC50 = 5400.0 nM 5.27 Inhibition of human cathepsin L 19665376
Cathepsin S IC50 = 5900.0 nM 5.23 Inhibition of human cathepsin S 19665376

Literature References

Data from ChEMBL 36 via Core Engine